ArticleMolecular nutrition & food research2017
Targeting the epigenome: Screening bioactive compounds that regulate histone deacetylase activity.
Article in Molecular nutrition & food research, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 46 citations in OpenAlex.
- Article
- Neuro-protective Potential of Honey: A Narrative Review.Current pharmaceutical design · 2026Review
- Histone Deacetylase Inhibition in Alzheimer's Disease: Molecular Mechanisms, Therapeutic Potential, and Future Perspectives.Current topics in medicinal chemistry · 2025Review
- The Contribution of Hippocampal All-Trans Retinoic Acid (ATRA) Deficiency to Alzheimer's Disease: A Narrative Overview of ATRA-Dependent Gene Expression in Post-Mortem Hippocampal Tissue.Antioxidants (Basel, Switzerland) · 2023Review
- The Potential Use of Honey as a Neuroprotective Agent for the Management of Neurodegenerative Diseases.Nutrients · 2023Review
- Nutritional Epigenetics in Cancer.Advances in nutrition (Bethesda, Md.) · 2022Review
- Review
- Quercetin alleviates diastolic dysfunction and suppresses adverse pro-hypertrophic signaling in diabetic rats.Frontiers in endocrinology · 2022Article
- The Effect of Acknowledged and Novel Anti-Rheumatic Therapies on Periodontal Tissues-A Narrative Review.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Functional Depletion of HSP72 by siRNA and Quercetin Enhances Vorinostat-Induced Apoptosis in an HSP72-Overexpressing Cutaneous T-Cell Lymphoma Cell Line, Hut78.International journal of molecular sciences · 2021Article
- Activators of alpha synuclein expression identified by reporter cell line-based high throughput drug screen.Scientific reports · 2021Article
- Flavonoid-based inhibition of cyclin-dependent kinase 9 without concomitant inhibition of histone deacetylases durably reinforces HIV latency.Biochemical pharmacology · 2021Article
- Divergent and Overlapping Roles for Selected Phytochemicals in the Regulation of Pathological Cardiac Hypertrophy.Molecules (Basel, Switzerland) · 2021Article
- The Anti-Inflammatory Properties of Phytochemicals and Their Effects on Epigenetic Mechanisms Involved in TLR4/NF-κB-Mediated Inflammation.Frontiers in immunology · 2021Review
- Article
- Dietary natural products as epigenetic modifiers in aging-associated inflammation and disease.Natural product reports · 2020Review
- Emodin and emodin-rich rhubarb inhibits histone deacetylase (HDAC) activity and cardiac myocyte hypertrophy.The Journal of nutritional biochemistry · 2020Article
- Molecular Mechanisms of Action of Emodin: As an Anti-Cardiovascular Disease Drug.Frontiers in pharmacology · 2020Review
- Deciphering the Anti-obesity Benefits of Resveratrol: The "Gut Microbiota-Adipose Tissue" Axis.Frontiers in endocrinology · 2019Review
- Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
scopeNutrigenomics is a rapidly expanding field that elucidates the link between diet-genome interactions. Recent evidence demonstrates that regulation of the epigenome, and in particular inhibition of histone deacetylases (HDACs), impact pathogenetic mechanisms involved in chronic disease. Few studies, to date, have screened libraries of bioactive compounds that act as epigenetic modifiers. This study screened a library of 131 natural compounds to determine bioactive compounds that inhibit Zn-dependent HDAC activity. METHODS AND
resultsUsing class-specific HDAC substrates, we screened 131 natural compounds for HDAC activity in bovine cardiac tissue. From this screen, we identified 18 bioactive compound HDAC inhibitors. Using our class-specific HDAC substrates, we next screened these 18 bioactive compounds against recombinant HDAC proteins. Consistent with inhibition of HDAC activity, these compounds were capable of inhibiting activity of individual HDAC isoforms. Lastly, we report that treatment of H9c2 cardiac myoblasts with bioactive HDAC inhibitors was sufficient to increase lysine acetylation as assessed via immunoblot.
conclusionThis study provided the first step in identifying multiple bioactive compound HDAC inhibitors. Taken together, this report sets the stage for future exploration of these bioactive compounds as epigenetic regulators to potentially ameliorate chronic disease.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.